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Flumatinib mesylate

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Catalog No. T7861Cas No. 895519-91-2
Alias HHGV678 mesylate

Flumatinib mesylate (HHGV678 mesylate) is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.

Flumatinib mesylate

Flumatinib mesylate

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Purity: 99.82%
Catalog No. T7861Alias HHGV678 mesylateCas No. 895519-91-2
Flumatinib mesylate (HHGV678 mesylate) is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$31In StockIn Stock
5 mg$81In StockIn Stock
10 mg$135In StockIn Stock
25 mg$263In StockIn Stock
50 mg$413In StockIn Stock
100 mg$662In StockIn Stock
500 mg$1,370-In Stock
1 mL x 10 mM (in DMSO)$142In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.82%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Flumatinib mesylate (HHGV678 mesylate) is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.
Targets&IC50
PDGFRβ:307.6 nM, c-ABL:1.2 nM
In vitro
In vivo study consistently suggested that flumatinib had superior efficacy compared with imatinib or sunitinib against 32D cells with the secondary mutation Y823D.?Molecular modeling of flumatinib docked to the KIT kinase domain suggested a special mechanism underlying the capability of flumatinib to overcome the drug-resistance conferred by activation loop mutations.?These findings suggest that flumatinib could be a promising therapeutic agent against GISTs resistant to both imatinib and sunitinib because of secondary mutations in the activation loop[1].
SynonymsHHGV678 mesylate
Chemical Properties
Molecular Weight658.69
FormulaC30H33F3N8O4S
Cas No.895519-91-2
SmilesCS(O)(=O)=O.CN1CCN(Cc2ccc(cc2C(F)(F)F)C(=O)Nc2cnc(C)c(Nc3nccc(n3)-c3cccnc3)c2)CC1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: 50 mg/mL (75.91 mM), Sonication is recommended.
DMSO: 70 mg/mL (106.27 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.04 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM1.5182 mL7.5908 mL15.1816 mL75.9082 mL
5 mM0.3036 mL1.5182 mL3.0363 mL15.1816 mL
10 mM0.1518 mL0.7591 mL1.5182 mL7.5908 mL
20 mM0.0759 mL0.3795 mL0.7591 mL3.7954 mL
50 mM0.0304 mL0.1518 mL0.3036 mL1.5182 mL
DMSO
1mg5mg10mg50mg
100 mM0.0152 mL0.0759 mL0.1518 mL0.7591 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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